TWI802604B - 嘧啶TBK/IKKε抑制劑化合物及其用途 - Google Patents

嘧啶TBK/IKKε抑制劑化合物及其用途 Download PDF

Info

Publication number
TWI802604B
TWI802604B TW107136567A TW107136567A TWI802604B TW I802604 B TWI802604 B TW I802604B TW 107136567 A TW107136567 A TW 107136567A TW 107136567 A TW107136567 A TW 107136567A TW I802604 B TWI802604 B TW I802604B
Authority
TW
Taiwan
Prior art keywords
amino
pyrimidin
methoxy
yloxy
compound
Prior art date
Application number
TW107136567A
Other languages
English (en)
Chinese (zh)
Other versions
TW201922735A (zh
Inventor
史瑞尼伐沙R 卡拉
玉方 肖
布萊恩A 雪倫
Original Assignee
德商默克專利有限公司
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 德商默克專利有限公司 filed Critical 德商默克專利有限公司
Publication of TW201922735A publication Critical patent/TW201922735A/zh
Application granted granted Critical
Publication of TWI802604B publication Critical patent/TWI802604B/zh

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Emergency Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW107136567A 2017-10-17 2018-10-17 嘧啶TBK/IKKε抑制劑化合物及其用途 TWI802604B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762573251P 2017-10-17 2017-10-17
US62/573,251 2017-10-17

Publications (2)

Publication Number Publication Date
TW201922735A TW201922735A (zh) 2019-06-16
TWI802604B true TWI802604B (zh) 2023-05-21

Family

ID=64110185

Family Applications (1)

Application Number Title Priority Date Filing Date
TW107136567A TWI802604B (zh) 2017-10-17 2018-10-17 嘧啶TBK/IKKε抑制劑化合物及其用途

Country Status (14)

Country Link
US (1) US20230019491A1 (enExample)
EP (1) EP3697772A1 (enExample)
JP (1) JP7266592B2 (enExample)
KR (1) KR20200072519A (enExample)
CN (1) CN111247135A (enExample)
AU (1) AU2018352699A1 (enExample)
BR (1) BR112020007466A2 (enExample)
CA (1) CA3078579A1 (enExample)
IL (1) IL273891A (enExample)
MX (1) MX2020003507A (enExample)
RU (1) RU2020115596A (enExample)
SG (1) SG11202003407VA (enExample)
TW (1) TWI802604B (enExample)
WO (1) WO2019079373A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11440899B2 (en) * 2017-10-17 2022-09-13 Merck Patent Gmbh Pyrimidine TBK/IKKe inhibitor compounds and uses thereof
KR102695210B1 (ko) 2018-06-05 2024-08-13 크리네틱스 파마슈티칼스, 인크. 멜라노코르틴 아형-2 수용체(mc2r) 길항제 및 이의 용도
CN112552280A (zh) * 2019-09-25 2021-03-26 常州强力先端电子材料有限公司 一种高产酸的磺酰亚胺类光产酸剂
WO2021091788A1 (en) * 2019-11-07 2021-05-14 Crinetics Pharmaceuticals, Inc. Melanocortin subtype-2 receptor (mc2r) antagonists and uses thereof
JP7672406B2 (ja) 2019-12-18 2025-05-07 クリネティックス ファーマシューティカルズ,インク. Gem-二置換ピペリジンメラノコルチンサブタイプ-2受容体(mc2r)アンタゴニストおよびその使用
JP7651574B2 (ja) 2019-12-23 2025-03-26 クリネティックス ファーマシューティカルズ,インク. スピロ環式ピペリジンメラノコルチンサブタイプ-2受容体(mc2r)アンタゴニストおよびその使用
BR112023018816A2 (pt) 2021-03-19 2023-10-31 Crinetics Pharmaceuticals Inc Antagonista do receptor de melanocortina subtipo-2 (mc2r) para o tratamento de doença
CN117447407B (zh) * 2023-12-19 2024-06-11 潍坊医学院 一种JAK2抑制剂Pacritinib及其中间体的制备方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011046970A1 (en) * 2009-10-12 2011-04-21 Myrexis, Inc. Amino - pyrimidine compounds as inhibitors of tbkl and/or ikk epsilon
WO2012142329A1 (en) * 2011-04-12 2012-10-18 Myrexis, Inc. Compositions and therapeutic uses of ikk-related kinase epsilon and tankbinding kinase 1 inhibitors
WO2013034238A1 (de) * 2011-09-09 2013-03-14 Merck Patent Gmbh Benzonitrilderivate als kinasehemmer

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2911139A1 (fr) * 2007-01-05 2008-07-11 Sanofi Aventis Sa Nouveaux derives de phenyl-(4-phenyl-pyrimidin-2-yl)amines, leur preparation a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de ikk
EP2200436B1 (en) * 2007-09-04 2015-01-21 The Scripps Research Institute Substituted pyrimidinyl-amines as protein kinase inhibitors
GB201012105D0 (en) * 2010-07-19 2010-09-01 Domainex Ltd Novel pyrimidine compounds
AU2016287335B2 (en) * 2015-06-29 2020-01-23 Merck Patent Gmbh TBK/IKKepsilon inhibitor compounds and uses thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011046970A1 (en) * 2009-10-12 2011-04-21 Myrexis, Inc. Amino - pyrimidine compounds as inhibitors of tbkl and/or ikk epsilon
WO2012142329A1 (en) * 2011-04-12 2012-10-18 Myrexis, Inc. Compositions and therapeutic uses of ikk-related kinase epsilon and tankbinding kinase 1 inhibitors
WO2013034238A1 (de) * 2011-09-09 2013-03-14 Merck Patent Gmbh Benzonitrilderivate als kinasehemmer

Also Published As

Publication number Publication date
MX2020003507A (es) 2020-07-22
EP3697772A1 (en) 2020-08-26
RU2020115596A3 (enExample) 2021-11-18
SG11202003407VA (en) 2020-05-28
RU2020115596A (ru) 2021-11-18
IL273891A (en) 2020-05-31
JP2020537671A (ja) 2020-12-24
AU2018352699A1 (en) 2020-05-28
CN111247135A (zh) 2020-06-05
US20230019491A1 (en) 2023-01-19
TW201922735A (zh) 2019-06-16
KR20200072519A (ko) 2020-06-22
CA3078579A1 (en) 2019-04-25
WO2019079373A1 (en) 2019-04-25
BR112020007466A2 (pt) 2020-09-24
JP7266592B2 (ja) 2023-04-28

Similar Documents

Publication Publication Date Title
JP7266592B2 (ja) ピリミジンTBK/IKKεインヒビター化合物およびそれらの使用
AU2015349899B9 (en) Heteroaryl compounds as IRAK inhibitors and uses thereof
US10428080B2 (en) TBK/IKK inhibitor compounds and uses thereof
JP7651590B2 (ja) アミノピリミジン誘導体およびアリール炭化水素受容体モジュレーターとしてのその使用
TWI802605B (zh) 嘧啶TBK/IKKε抑制劑化合物及其用途
HK40086197A (en) Aminopyrimidine derivatives and their use as aryl hydrocarbon receptor modulators
HK1242303A1 (en) Heteroaryl compounds as irak inhibitors and uses thereof
HK1242303B (en) Heteroaryl compounds as irak inhibitors and uses thereof

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees